Enhanced skin deposition and delivery of voriconazole using ethosomal preparations

Abstract

Despite its broad-spectrum antifungal properties, voriconazole has many side effects when administered systemically. The aim of this work was to develop an ethosomal topical delivery system for voriconazole and test its potential to enhance the antifungal properties and skin delivery of the drug. Voriconazole was encapsulated into various ethosomal preparations and the effect of phospholipid and ethanol concentrations on the ethosomes properties were evaluated. The ethosomes were evaluated for drug encapsulation efficiency, particle size and morphology and antifungal efficacy. Drug permeability and deposition were tested in rat abdominal skin. Drug encapsulation efficiency of up to 46% was obtained and it increased with increasing the phospholipid concentration, whereas the opposite effect was observed for the ethanol concentration. The ethosomes had a size of 420-600 nm and negative zeta potential. The particle size of the ethosomes increased by increasing their ethanol content. The ethosomes achieved similar inhibition zones against Aspergillus flavus at a 2-fold lower drug concentration compared with drug solution in dimethyl sulfoxide. The ex vivo drug permeability through rat abdominal skin was ∼6-fold higher for the ethosomes compared with the drug hydroalcoholic solution. Similarly, the amount of drug deposited in the skin was higher for the ethosomes and was dependent on the ethanol concentration of the ethosomes. These results confirm that voriconazole ethosomal preparations are promising topical delivery systems that can enhance the drug antifungal efficacy and improve its skin delivery.

Liposomal and Ethosomal Gels for the Topical Delivery of Anthralin: Preparation, Comparative Evaluation and Clinical Assessment in Psoriatic Patients

“…Zhang et al, showed that the transdermal flux and skin deposition of psoralen-loaded ethosomes were 3.5 and 2.15 times higher than those achieved using liposomes, respectively [28]. We also showed that ethosomes had~6-fold higher voriconazole permeation through rat abdominal skin compared with the drug hydroalcoholic solution [29]. These results suggest that ethosomes could be a potentially effective delivery system to increase anthralin efficacy against psoriasis and limit its adverse effects.…”

“…Anthralin-loaded ethosomes were prepared by the cold method as described previously with some modifications [29,32]. Table 2 shows the different components of ethosomes and their proportions.…”

“…These studies were carried out using rat abdominal skin according to previously published procedures [29,37]. The abdominal skin was obtained from Wistar male albino rats (6-8 weeks old) weighing 90-100 g. All animals were treated in accordance with the ethical guidelines approved by Faculty of Pharmacy, Assiut University (ethical approval number: S4-19, 1-9-2019), which follows the Guide for the Care and Use of Laboratory Animals, 8th Edition, National Academies Press, Washington, DC.…”

Preparation and Optimization of Buccal Propranolol Hydrochloride Nanoethosomal Gel: A Novel Approach for Enhancement of Bioavailability

“…The drug is supposed to be entrapped in the aqueous compartment of the vesicles, and the decrease in the EE may be attributed to the increase in the fluidity of vesicles upon increase in the ethanol content leading to drug leakage [33]. Vesicle size had direct relationship with PC and negative relation with PG and ethanol these results were in agreement with the reported results [32,34]. The size reduction with increasing PG and ethanol could be attributed to negatively charge by ethanol which causes electrostatic repulsion and some degree of stearic stabilization.…”

Spironolactone-Loaded LeciPlexes as Potential Topical Delivery Systems for Female Acne: In Vitro Appraisal and Ex Vivo Skin Permeability Studies

“…This size is smaller than that obtained by DLS measurements (Table 2), since DLS measurements give the hydrodynamic diameter of the nanoparticles, which is usually larger than the actual particle size. In contrast, TEM measurements give the size of the vesicles after drying [50]. Figure 4 shows the in vitro SP release from various formulations in phosphate-buffered saline pH 7.4.…”